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41 Cards in this Set
- Front
- Back
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What are the 3 major Sex Steroids?
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Estrogen
Progestins Androgens |
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What is the MOA of Sex Steroids?
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1. They enter the cell
2. They bind to Cystosolic receptor forming a Complex 3. The complex formed moves to the nucleus 4. In the nucleus they activate gene transcription |
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What is the function of estrogen in females?
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Estrogen is involved in the
-development of female sex organs -regulation of the menstrual cycle |
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What are the 3 Estrogens produced by the female body?
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Estradiol
Estrone Estriol |
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Which is Most potent of the 3?
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Estradiol- principal secretory product from Ovaries
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What are the precursors of Estrogen synthesis?
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Androstendione
Testosterone |
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Name some other physiological functions of Estrogen
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Stimulates endometrial growth
-reduces bone resorption -maintains structure of skin and blood vessels -increases thyroxin -binding globin -increases HDL and TAG levels -decreases LDL levels -Promotes coagulation of blood |
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What are the estrogens used clinically?
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-Estradiaol (Estrace)
-Conjugated Estrogen (Premarin) -from pregnant mare's urine) -Ethynyl estradiol (Estinyl) -undergoes less 1st pass metabolism Quinestrol (Estrovis) -synthetic, NON-steroidal Either given Orally, IM or Transdermally |
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What r the clinical uses of Estrogens?
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-Treatmont of hypogonadism in girls
-as Oral conraceptive in combo with Progestins -HRT in post-menopausal women -Treatment of PROSTATE CA. -Useful for Acne and dysmenorrhea |
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Potential TOXIC effects of Estrogens?
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Long term use causes
HTN -Thromboembolism -hepatic adenoma -Breast and endometrial Ca It also causes Breast tenderness Endometrial Hyperplasia Migraine Cholestasis C/I in Pregnancy Liver disease Breast CA H/o Thormboembolism |
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What is the effect of Estogens on clotting factors?
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It decr. antithrombin III
At HIGH doses , it incr. Factors II,VII,IX and X |
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What is the MOA of SERMs- Selective estrogen receptor modulator?
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The are antagonists in some tissues and agonists in others
Used in treatment of Breast CA in PostM women Prophylaxis in high risk cases of Breast CA Acts as an antagonist to prevent receptor activation by endogenous estrogen |
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Give the names of the SERMs?
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TAMOXIFEN
RALOXIFENE Toremifene |
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What is the use of the agonist action in SERMs?
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Prevent osteoporosis
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A/E of SERMs
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N +V, hot flushes, Thrombosis
TAMOXIFEN -acts as an agonist at the Endometrial receptors -RISK of endometrial CA RALOXIFENE-has no such effect on endometrium |
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What is CLOMIPHENE?
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An Estrogen ANTAGONIST in Hypothalmus and at. Pituitary
An Estrogen AGONIST Ovary Clomiphene works at the level of the hypothalamus where it competes for estrogen binding sites. When these "sites are occupied", the hypothalamus responds by producing more GnRH which then stimulates the pituitary to produce FSH and LH leading to stimulation of the ovary |
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What is the clinical use of Clomiphne?
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Treatment of infertility
A/E Multiple births, hot flashes, visual disturbances, ovarian enlargement |
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What is the precursor for progestin-Progesterone?
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Cholesterol
Progesterone is synthesized in the: Ovary Testis Adrenal gland |
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Name the physiological functions of Progesterone?
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Stimulates LPL activity and incr. fat deposition
-decr. insulin response to glucose -decr. uterin contractility -decr gallbladder contraction -regulate endometrium secretory phase -regulate the development of breast secretory glands |
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What is Medroxyprogesterone acetate -Provera?
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Synthetic Progestin
Others: Norethindrone (Norlutin) Norethindrone acetate (Aygestin) |
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What are the therapeutic uses of Progestins?
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CONTRACEPTION -used alone or in combo with Estradiol
HRT- in combo with Estrogen Treatment of : Dysmenorrhea, Endometriosis Diagnosis of: Estrogen secretion in Amenorhea (if menstruation occurs after giving progesterone then the uterus HAS BEEN stimulated by Estrogen |
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What are the AE of Progestins?
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Weight gain
Depression (mjr) Edema Acne, Hirsutism Hypertention Pulmonary Embolism Thrombophlebitis Admin: Oral or IM injection Cholestatic Jaundice |
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What is the 'morning after' pill?
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A Competitive Inhibitor of progesterone receptor
MIFEPRISTONE (RU 486 - used as an Abortifacient Given concomitantly with PGE or PGF - to increase myometrial contraction |
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What are the AE of MIFEPRISTONE?
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Excessive bleeding
GI effects - Nausea, vomiting, Anorexia, abdominal pain |
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Name a Partial AGONIST at Progesterone recptors?
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DANAZOL -(danocrine)
Also a Partial Agonist at Androgen and Glucocorticoid receptors |
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What is the clinical use of Danozol?
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Treatment of ENDOMETRIOSIS
(anti-proliferative effect by negative feed-back) AE -Wt gain, Edema, Acne, decr. HDL levels |
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What are Androgens derived from?
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Cholesterol
Androgens are steroids |
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Name the androgens produced by the testis.
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Testosterone
Dihydrotestosterone De-hydro-epi-androsterone DHEA (I only broke it up to spell it right) Androstendione Principal androgen is TESTOSTERONE - |
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Name the precursors of Testosterone.
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Produced from Progesterone and DHEA
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Name 2 other glands where testosterone is produced.
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Adrenal gland and Ovary
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What are the physiologic effects of androgens?
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Anabolic effects - incr. in muscle mass and RBC procuction
Androgenic effects - Growith of skeleton, larynx, facial hair and darkening skin |
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Name 6 Synthetic Androgens.
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Oxandrolone
Oxymetholone Fluoxymestrone Stanozolol Nandrolone Phenpropionate |
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Give the clinical uses of Androgens.
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-Used in males with hypogonadism (inadequate androgen secretion)
-Osteoporosis in elderly -Growth stimulation - bone growth in pre-pubertal boys with pituitary dwarfism -Incr muscle mass |
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What toxic effects occur with androgens?
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Over- Masculinization
In women - Hirsutism, Depression of menses, Acne, clitoral enlargement *Cholestatic jaundice, *Prostatic hypertrophy *Premature closure of epiphysis ( may lead to dependence) Rarely - Hepatic CA and adenomas, |
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Is treatment with androgens safe in pregnancy ?
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NO
can lead to virilization in Female fetus |
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Androgen ANTAGONISTS are divided into four categories namely.....
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1. Gonadotropin releasing analogues - LEUPROLIDE or GONADORELIN
2. Receptor Inhibitors - FLUTAMIDE, CYPROTERONE, SPIRINOLACTONE 3. Steroid synthesis inhibitors: KETOCONAZOLE 4. 5- alpha reductase inhibitors -FINASTRIDE (pROPECIA) |
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What Androgen Antagonist is used in BPH ( benign prostatic hyperplasia)?
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FINASTRIDE
Reduces the production of DHT |
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What Androgen Antagonist is used in Hirsutism?
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Cyproterone and Spirinolactone
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What Androgen Antagonist is used in Prostatic CA?
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LEUPROLIDE
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Ketoconazole (steroid synthesis inhibitor) is used in which endocrine disease?
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Cushing's disease
Yes! Ketoconazole is an antifungal drug |
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Thats enough
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The end
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